药用辅料羟丙基纤维素在制剂中的应用

目的综述羟丙基纤维素在制剂中的应用,以促进在此方面的研究和开发。方法查阅有关文献,进行分析总结。结果羟丙基纤维素在片剂、胶囊剂、黏膜黏附制剂、缓控释制剂等多种制剂以及薄膜包衣方面均有良好应用。结论羟丙基纤维素是一种性能全面、应用广泛,具有远大前景的药用辅料。     

药用辅料羟丙基纤维素在制剂中的应用

目的综述羟丙基纤维素在制剂中的应用,以促进在此方面的研究和开发。方法查阅有关文献,进行分析总结。结果羟丙基纤维素在片剂、胶囊剂、黏膜黏附制剂、缓控释制剂等多种制剂以及薄膜包衣方面均有良好应用。结论羟丙基纤维素是一种性能全面、应用广泛,具有远大前景的药用辅料。     

羟丙基纤维素在片剂方面的应用

目的：综述羟丙基纤维素在片剂方面的应用，以促进在此方面的研究开发。方法：查阅有关献，进行分析总结。结果：羟丙基纤维素在片剂方面的应用，主要侧重于三方面：用于提高片剂质量；用于速释固体制剂；用于缓释、控释片制剂。结论：羟丙基纤维素可以提高片剂质量，解决片剂生产中的许多老大难问题，而且其在速释片剂和缓释、控释片剂方面的应用，使其更具生命力。羟丙基纤维素是一种具有远大前景的优良的药用辅料。     

羟丙基甲基纤维素眼用粘弹剂的制备和临床应用

目的:按照军队医疗单位非标准制剂技术要求进行2%羟丙基甲基纤维素的研制.方法:对该制剂的处方组成、制备工艺、质量控制及临床应用进行试验和总结.结果:该制剂配方和制备工艺合理,质量控制方法可行,能满足眼科手术的临床要求,使用情况良好.结论:2%羟丙基甲基纤维素是安全有效的眼用粘弹剂.     

亲水凝胶在药物制剂中的应用

羟丙基甲基纤维素及卡泊波树脂遇水后均可形成亲水凝胶,在缓释制剂中通过亲水凝胶层控制药物的释放。本文影响亲水凝胶控制药物释放的因素如辅料本身的性质,药物的性质以及介质等进行了综术,并着重介绍了羟丙基甲基纤维素在骨架制剂和包衣中的作用,以及卡泊波树脂在固体缓释制剂和口服蛋白给药系统中的应用及最新进展。     

羟丙甲纤维素在固体制剂应用中的研究进展

羟丙甲纤维素(HPMC)作为一种多功能辅料,在片剂、缓释与控释制剂、胶囊等固体制剂中已被广泛应用。本文从片剂、缓释与控释制剂、胶囊等方面出发,举例介绍了羟丙甲纤维在固体制剂中的具体应用情况。     

羟丙甲纤维素在外用混悬型制剂中的应用

羟丙甲纤维素(hypromellosem,HPMC)是具有优良性能的羟丙基与甲基以醚键连接的纤维素衍生物,为类白色纤维状粉末,在水中溶解形成澄明具有粘性的胶体溶液。此特性大大增加了它在制剂中的应用空间。该产品与多数药物不产生反应,是一种中性的并对人体无害的纤维素衍生物。 混悬型液体制剂是临床上的常用剂型,为难溶性固体药物分散在液体分散介质中形成的非均相分散体系。该体系的稳定性决定了混悬型液体制剂质     

羟丙甲基纤维素在药剂学中的应用

根据羟丙甲基纤维素的性质、特点,探讨其在片剂、缓释与控释剂、眼部给药系统、混悬型液体制剂、凝胶和软膏等7个方面的作用,并就近年来羟丙甲基纤维素在药剂学领域中的应用作一回顾.     

西罗莫司缓释片的制备及其释药因素考察

目的制备西罗莫司缓释片并对其释药因素进行考察。方法采用羟丙基甲基纤维素（HPMC）为基本骨架材料制备了西罗莫司凝胶骨架片,对影响释药的因素,如采用羟丙基甲基纤维素（HPMC）规格、用量、填充剂种类、致孔剂用量、压片压力及释放介质等进行了考察。结果以30%羟丙基甲基纤维素（HPMC K4M）为骨架材料、2%乳糖为致孔剂、微晶纤维素（MCC）为填充剂时,缓释片呈明显一级释放特征。结论该制剂在体外具有良好的缓释效果,且制备工艺简单易行。     

羟丙甲纤维素衍生物研究概述

目的：了解羟丙甲纤维素衍生物的研究概况,为药用新辅料及新剂型的研究提供参考。方法：通过查阅中国期刊网和万方数据库2001-2012年国内外相关文献资料,从材料角度对羟丙甲纤维素衍生物的制备方法、结构确认、性能以及在药物制剂中的应用等方面进行综述。结果与结论：羟丙甲纤维素衍生物能显著提高药物的生物利用度和靶向性。作为新型药用辅料,已广泛应用于肠溶制剂、缓控释制剂和结肠处药物定位释放给药系统的包衣材料,为药物制剂新剂型提供了新型辅料,在药物新剂型的研制方面发挥着重要作用。     

羟丙甲纤维素酞酸酯水分散体的制备及表征

用乳化溶剂蒸发法制备了羟丙甲纤维素酞酸酯水分散体.结果表明其平均粒径215nm,分布均匀,并具有良好的稳定性和成膜性能.     

流化床制粒法制备甲磺酸吉米沙星片

目的：探索流化床制粒法制备甲磺酸吉米沙星片的工艺参数。方法：以崩解时限为指标,对甲磺酸吉米沙星片的处方进行筛选。结果：500g甲磺酸吉米沙星,60gMCC作为填充剂,600m15％HPMC溶液作为黏合剂,20gCMS—Na作为崩解剂．可制得的颗粒能够制备崩解性能良好的片剂。结论：流化床制粒法解决了传统湿法制粒制备甲磺酸吉米沙星片所遇到的困难。     

Dissolution rate studies of compression-molded units made from hydroxypropyl cellulose films

Hydroxypropyl cellulose films were prepared by compression molding of three different lots of hydroxypropyl cellulose powder at 149 degrees C, 188 degrees C, and 232 degrees C. Rectangular pieces were cut from these films and viscosity average molecular weight (Mv), degree of orientation, and rate of dissolution were measured. The viscosity average molecular weight (Mv) decreased with increasing processing temperature, while, as expected, the dissolution rate increased. Orientation in the thermoformed units was also evaluated. Correlation of these data with the Mv values suggests that orientation has some controlling influence on the dissolution rate. Because the samples possessing the least orientation were molded at the highest temperature, they also had the lowest Mv due to thermal degradation. Therefore, the effects of molecular weight were not fully separated from orientation effects with regard to control over the dissolution rate.     

Effect of fixed aqueous layer thickness of polymeric stabilizers on zeta potential and stability of aripiprazole nanosuspensions

The aim of this study was to evaluate the effect of the thickness of adsorbed polymer layer (also known as Fixed Aqueous Layer Thickness, FALT) of polymeric stabilizers on zeta potential and stability of nanoparticles in a suspension. Aripiprazole, a poorly water soluble drug was used as a model drug to evaluate rationale for increased FALT and to understand the effect of hydrophilicity and hydrophobicity of polymeric stabilizers on FALT of aripiprazole nanosuspensions. The nanosuspensions were prepared by media milling and Pluronic F68, Pluronic F127, Hydroxypropyl methylcellulose (HPMC) and Hydroxypropyl cellulose (HPC) were used as polymeric stabilizers. The particle size (immediately after preparation and after 1 week of storage at 25°C) and zeta potential of aripiprazole nanosuspensions were determined. For Pluronics, FALT was determined theoretically whereas for HPMC and HPC it was calculated as Debye Huckel parameter from the zeta potential dependence on the ionic strength. An increase in FALT resulted in reduced zeta potential. With an increase in FALT of polymers used, the stability of nanosuspensions showed improvement. Furthermore, a linear correlation was shown to exist between the FALT and length of hydrophilic chains in Pluronics.     

利用海带渣制备药用辅料微晶纤维素的研究

目的为了高效利用海洋生物资源,降低环境污染,以海带加工废弃海带渣为原料制备药用辅料微晶纤维素。方法利用海带渣纤维素与HCl进行水解反应制备微晶纤维素,并研究反应时间对微晶纤维素制备的影响。利用扫描电子显微镜观察微晶纤维素的形貌,利用X射线衍射仪分析微晶纤维素的物相组成的表征。测定产品和市售样品的溶胀性,并将产品和市售样品以阿司匹林为主药进行压片,按照中国药典的规定对其进行硬度、崩解度、溶出度对比考察。结果在酸料比为1∶10,,盐酸浓度为2mol.L-1,水解温度为100℃的条件下,最佳水解时间为40min。海带渣微晶纤维素呈不规则的颗粒状,结晶度为79%,晶粒尺寸为3.9nm。与市售样品相比较,产品压片后崩解时限短、溶出速度快。结论以海带渣为原料用于药用辅料微晶纤维素的制备是可行的,所制备的微晶纤维素性能良好。     

Safety assessment of hydroxypropyl methylcellulose as a food ingredient

Hydroxypropyl methyl cellulose (HPMC; CAS No. 9004-65-3) is an odorless and tasteless, white to slightly off-white, fibrous or granular, free-flowing powder that is a synthetic modification of the natural polymer, cellulose. It is used in the food industry as a multipurpose food ingredient. HPMC is approved by FDA as both a direct and an indirect food additive, and is approved for use as a food additive by the EU. The JECFA has evaluated the food uses of HPMC and established an acceptable daily intake (ADI) of ‘not specified’ for such uses. Based on the no-observed-adverse-effect level (NOAEL) of 5000 mg/kg body weight/day from a 90-day feeding study in rats, a tolerable intake for ingestion of HPMC by humans of 5 mg/kg body weight/day is posited and, as such, is more than 100-fold greater than the estimated current consumption of 0.047 mg/kg body weight/day.     

丹皮酚磺酸钠即型凝胶角膜透过性及其对小鼠免疫性结膜炎治疗作用

目的：考察丹皮酚磺酸钠眼用即型凝胶的角膜透过能力,并对其治疗小鼠免疫性结膜炎作用进行评价。方法：以卡波姆为凝胶基质,羟丙甲基纤维素为增稠剂,采用改良Franz扩散池,对丹皮酚磺酸钠眼用即型凝胶的角膜透过性进行测定,并建立小鼠免疫性结膜炎模型,以肥大细胞脱颗粒情况、IL-4、OVA-sIgE为指标,评价该眼用凝胶的药效。结果：丹皮酚磺酸钠pH敏感眼用凝胶能显著促进药物角膜透过性,抑制肥大细胞脱颗粒,下调小鼠血清中IL-4、OVA-sIgE作用。结论：丹皮酚磺酸钠眼用即型凝胶对小鼠免疫性结膜炎具有治疗作用。     

甲砜霉素缓释片的制备及释放度研究

目的以甲砜霉素为模型药物,考察缓释片的处方及工艺因素对其体外释放的影响。方法以羟丙基甲基纤维素为骨架材料,预胶化淀粉等为填充剂,以体外释放度为指标考察处方及工艺因素对药物溶出度的影响。结果按最优处方制得的缓释片体外释放满足要求;甲砜霉素缓释片的释药过程通过Peppas方程拟合,初步说明甲砜霉素从骨架中的释放是扩散和溶蚀综合作用的结果。结论该缓释片处方设计合理,工艺重现性好,缓释效果好,适合工业生产。     

Matrix-type transdermal drug delivery system of trandolapril: in vitro and ex vivo characterization

The purpose of the investigation was to develop and evaluate matrix-type transdermal drug delivery systems (TDDSs) of trandolapril. Matrix-type TDDSs of trandolapril were prepared by solvent evaporation technique. Eight formulations (composed of Eudragit RL 100 and Hydroxypropyl methyl cellulose 15 cps at a ratios of 2:8, 4:6, 6:4, 8:2 in formulations A1, A2, A3, A4; and Eudragit RS 100 and Hydroxypropyl methyl cellulose 15 cps in the same ratios in formulations B1, B2, B3, B4, respectively) were prepared. All formulations contained 5% w/w menthol as penetration enhancer and 15% w/w propylene glycol as plasticizer in ethanol as solvent. The prepared TDDSs were evaluated for physicochemical characteristics, in vitro release and ex vivo permeation. The physicochemical interactions between trandolapril and polymers were investigated by Fourier transform infrared spectroscopy. The results suggested that there is no physicochemical interaction between drug and polymers. The maximum drug release in 24 h for A series formulations was 95.45% (A1), 95.82% (A2), and it was 95.26% (B1), 95.69% (B2) for B series formulations, which are significantly (P < 0.05) different than the lowest values 78.79% (A3), 66.9% (A4) and 82.64% (B3), 71.67% (B4). The formulations A1 (flux 25.03 ± 0.98 μg/cm(2)/h) and B1 (flux 24.62 ± 0.63 μg/cm(2)/h) showed maximum skin permeation in the respective series. The flux obtained with formulations A1 and B1 meets the required flux (37.04 μg/h/cm(2)) with a minimum patch area (3.9 cm(2)). Matrix-type transdermal therapeutic systems of trandolapril could be prepared with the required flux using menthol as penetration enhancer.